S3319
sPLA2抑制剂
别名:
5-(4-苄氧基苯基)-4S-(7-苯基庚酰基氨基)戊酸, KH064
方案
≥97.5% (HPLC)
表单
powder
储存条件
under inert gas
颜色
white
mp
133-135 °C
溶解性
DMSO: 20 mg/mL, clear
储存温度
2-8°C
SMILES字符串
OC(=O)CC[C@@H](Cc1ccc(OCc2ccccc2)cc1)NC(=O)CCCCCCc3ccccc3
InChI
1S/C31H37NO4/c33-30(16-10-2-1-5-11-25-12-6-3-7-13-25)32-28(19-22-31(34)35)23-26-17-20-29(21-18-26)36-24-27-14-8-4-9-15-27/h3-4,6-9,12-15,17-18,20-21,28H,1-2,5,10-11,16,19,22-24H2,(H,32,33)(H,34,35)/t28-/m0/s1
InChI key
KWLUIYFCMHKLKY-NDEPHWFRSA-N
应用
sPLA2抑制剂已被用于研究对于肺癌细胞和少突胶质细胞增殖和凋亡的影响。
分泌型磷脂酶A2抑制剂已用于：
- 人肺腺癌细胞的Matrigel侵袭实验
- 预处理培养的少突胶质细胞
- 抑制肺腺癌的分泌型磷脂酶A2。
生化/生理作用
sPLA2抑制剂（pla2g2a）是一种具有口服活性、有效的分泌型磷脂酶A2（sPLA2；组IIa）抑制剂。分泌型磷脂酶A2抑制剂可阻断NF-KB、Akt、p38 MAPK以及ERK通路的激活。sPLA2抑制剂可减少肺癌细胞的增殖并诱导其凋亡，是一种有效的抗炎剂。sPLA2抑制剂可防止胶原沉积，并在高血压大鼠中具有抗纤维化作用。
分泌型磷脂酶A2(sPLA2)抑制剂是分子量为487.63 Da的亲脂性分子。它调节炎症反应和脂蛋白功能，可用于治疗动脉粥样硬化。
分泌型磷脂酶A2抑制剂可阻断NF-κB、Akt、p38 MAPK以及ERK通路的激活。 它可减少肺癌细胞的增殖并诱导其凋亡，是一种有效的抗炎剂。 sPLA2抑制剂可防止胶原沉积，并在高血压大鼠中具有抗纤维化作用。
口服活性，有效的分泌型磷脂酶A2（sPLA2；组IIa）抑制剂。
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
个人防护装备
Eyeshields, Gloves, type N95 (US)
法规信息
新产品
此项目有
Jessica A Yu et al.
Anticancer research, 32(9), 3601-3607 (2012-09-21)
Group IIa secretory phospholipase A2 (sPLA2 IIa) has been implicated in the regulation of metastasis of non-small cell lung cancer (NSCLC) and the present study investigates its contribution to lung cancer growth and progression. PLA2s initiate signaling in several pathways
Scott Levick et al.
Journal of immunology (Baltimore, Md. : 1950), 176(11), 7000-7007 (2006-05-20)
The development of fibrosis in the chronically hypertensive heart is associated with infiltration of inflammatory cells and cardiac hypertrophy. In this study, an inhibitor of the proinflammatory enzyme, group IIA human secretory phospholipase A2 (sPLA2-IIA), has been found to prevent
Differential expression of sPLA2 following spinal cord injury and a functional role for sPLA2-IIA in mediating oligodendrocyte death
Titsworth WL, et al.
Glia, 57(14), 1521-1537 (2009)
Discovery of AZD2716: a novel secreted phospholipase A2 (sPLA2) inhibitor for the treatment of coronary artery disease
Giordanetto F, et al.
ACS Medicinal Chemistry Letters, 7(10), 884-889 (2016)
Robert C Reid
Current medicinal chemistry, 12(25), 3011-3026 (2005-12-28)
Phospholipases A2 cleave membrane phospholipids to release arachidonic acid, the precursor to a large family of pro-inflammatory eicosanoids including prostaglandins and leukotrienes that have been proven to exacerbate numerous diseases that have an inflammatory component. Current therapies include NSAIDs' that
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